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首页> 外文期刊>Cardiology in review >Bempedoic Acid (ETC-1002): ATP Citrate Lyase Inhibitor Review of a First-in-Class Medication with Potential Benefit in Statin-Refractory Cases
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Bempedoic Acid (ETC-1002): ATP Citrate Lyase Inhibitor Review of a First-in-Class Medication with Potential Benefit in Statin-Refractory Cases

机译：Bempedo酸（ETC-1002）：ATP柠檬酸盐酶抑制剂综述患有他汀类药物难治性案件的潜在益处的一级药物

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摘要

Bempedoic acid (BA; ETC-1002) is a new agent that reduces cholesterol synthesis through inhibition of adenosine triphosphate citrate lyase, an enzyme upstream from 3-hydroxy-3-methylglutaryl-coenzyme A. In animal models, BA also influences fatty acid synthesis, but in humans, its role is limited primarily to lowering low-density lipoprotein cholesterol (LDL-C). In early clinical trials, BA was well tolerated and without major side effects. Alone or in various combinations with atorvastatin and/or ezetimibe, LDL-C lowering ranged from 17% to 64%. In addition, BA lowers levels of non-high-density lipoprotein cholesterol, C-reactive protein, and apolipoprotein B. Statins are first-line agents for primary and secondary prevention of cardiovascular disease. However, muscle-related side effects and other problems such as elevated liver enzymes may limit their use. In addition, LDL-C lowering beyond that provided by statin therapy alone may be needed. BA may be useful in either of these scenarios, as it is relatively free of muscle-related side effects and appears to enhance LDL-C lowering beyond that achieved with statin monotherapy. Phase 3 trials and one outcomes study are currently under way to better define this agent's potential clinical role.
机译：Bempedo酸（BA; ETC-1002）是一种通过抑制腺苷三磷酸柠檬酸酯裂解酶的胆固醇合成的新试剂，从3-羟基-3-甲基戊齐芳基 - 辅酶A上游。在动物模型中，BA也影响脂肪酸合成但在人类中，其作用主要是限于降低低密度脂蛋白胆固醇（LDL-C）的限制。在早期的临床试验中，BA耐受良好，没有主要的副作用。单独或以与阿托伐他汀和/或ezetimibe的各种组合，LDL-C降低的范围从17％到64％。此外，BA降低了非高密度脂蛋白胆固醇，C-反应性蛋白和载脂蛋白B的水平。他汀类药物是用于初级和二次预防心血管疾病的一线剂。然而，肌肉相关的副作用和诸如肝酶升高的其他问题可能限制它们的使用。此外，可能需要单独降低超出其单独提供的Satisin治疗提供的LDL-C。 BA可能在这些场景中有用，因为它相对不含肌肉相关的副作用，并且似乎增强了通过他汀类药物单疗法实现的LDL-C降低。目前正在进行第3阶段试验和一个结果研究，以更好地定义该代理的潜在临床作用。

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